This invention generally pertains to heterocyclic carbon compounds having drug and bio-affecting properties and to their preparation and use. In particular, the invention is concerned with 1,4-disubstituted piperazine derivatives wherein one substituent is 1,2-benzisothiazol-3-yl, unsubstituted or substituted in its benzoring; and the other substituent is, inter alia, alkyl, cycloalkyl, aralkyl, and phenoxyalkyl.
Related art may be viewed in light of the following general structural Formula I ##STR2## in which R and Z are substituents and X is a hetero ring atom or grouping. The most closely related art appears to be that contained in two issued patents assigned to Bristol-Myers and Company.
In U.S. Pat. No. 4,411,901, issued on Oct. 25, 1983, to Temple and Yevich, a series of neuroleptic agents of structure 2 is disclosed ##STR3## wherein Z is hydrogen or halogen and R represents the radical: ##STR4## and n is 3 or 4. As can be seen, the R- substituents a-d are heterocyclic rings, whereas incorporation of e and f into structure `produces antipsychotic butyrophenone derivatives. A synthetic intermediate compound (3) was also disclosed ##STR5## and was claimed in the related divisional U.S. Pat. No. 4,452,799, issued June 5, 1984.
A series of compounds disclosed as anti-inflammatory agents by Wade and Kissick in U.S. Pat. No. 4,104,388, issued Aug. 1, 1978, have structural formula 4. ##STR6## wherein Y can be C or N; A is a single bond or a 1-4 carbon alkylene chain; and B is hydrogen, hydroxyl, or optimally substituted phenyl. These compounds are easily distinguished as they are 1,1-dioxide ring derivatives of benzisothiazole.
The following references, while related, are less relevant to the new compounds disclosed in this application.
Strupczewski, et al, in U.S. Pat. No. 4,355,037, issued Oct. 19, 1982, disclosed a series of benzisoxazolyl piperidine derivatives (5) described as analgetic agents. ##STR7## In structure (5), R can be hydrogen, alkyl, alkenyl, cycloalkylalkyl, phenalkyl, hydroxy, aminoalkyl, cyano, cyanoalkyl, alkanolyl, or a carboxylic acid ester moiety.
Even further removed is a series of benzisoxazole-piperidine compounds shown as structure 6 ##STR8## which were disclosed as anti-psychotics and analgesics by Davis and Klein in U.S. Pat. No. 4,396,770, issued Aug. 2, 1983.
As can be seen, there is nothing in the foregoing references concerning related art which would suggest or make obvious the compounds of the present invention.